Claims
- 1. A compound of the formula: ##STR8## wherein R.sup.1 is amino,
- R.sup.2 is hydrogen,
- R.sup.3 is carboxy,
- R.sup.4 is unsaturated 3 to 8-membered 1 to 3 N-containing heteromonocyclic (lower) alkenyl, unsaturated 3 to 8-membered 1 to 3 N-containing heteromonocyclic (lower) alkenylthio, unsaturated 3 to 8-membered 1 to 3 N-containing heteromonocyclic (lower) alkenylthio, unsaturated 3 to 8-membered 1 to 3 N-containing heteromonocyclic thio(lower) alkylthio in each of which heteromonocyclic groups may be substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy and cyano, and
- R.sup.5 is halogen and pharmaceutically acceptable salts thereof.
- 2. A method for the treatment of bacterial infectious diseases which comprises administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a human or an animal.
- 3. A compound of claim 1, wherein
- R.sup.4 is pyridyl (lower) alkenyl, pyridyl (lower) alkenylthio or triazolylthio (lower) alkylthio.
- 4. A process for preparing a compound of the formula: ##STR9## wherein R.sup.1 is amino,
- R.sup.2 is hydrogen,
- R.sup.3 is carboxy,
- R.sup.4 is unsaturated 3 to 8-membered 1 to 3 -N-containing heteromonocyclic (lower) alkenyl, unsaturated 3 to 8-membered 1 to 3 -N-containing heteromonocyclic (lower) alkenylthio, unsaturated 3 to 8-membered 1 to 3 -N-containing heteromonocyclic thio(lower) alkylthio in each of which heteromonocyclic groups may be substituted with substituent(s) selected from the group-consisting of lower alkyl, hydroxy and cyano,
- R.sup.5 is a halogen or salts thereof, which comprises
- (1) reacting a compound of the formula: ##STR10## wherein R.sup.3 and R.sup.4 are each as defined above, or its reactive derivative at the amino group, or a salt thereof with a compound of formula: ##STR11## wherein R.sup.1, R.sup.2, and R.sup.5 are each as defined above, or its reactive derivative at the carboxy group, or a salt thereof, to give a compound of the formula: ##STR12## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined above, or a salt thereof, or
- (2) subjecting a compound of the formula: ##STR13## wherein R.sup.1, R.sup.3, R.sup.4 and R.sup.5 are each as defined above, and R.sup.2.sub.a is hydroxy protective group, or a salt thereof, to an elimination reaction of the hydroxy protective group, to give a compound of the formula: ##STR14## wherein R.sup.1, R.sup.3, R.sup.4 and R.sup.4 are each as defined above, or a salt thereof, or
- (3) subjecting a compound of the formula: ##STR15## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each as defined above, R.sup.3.sub.a is protected carboxy or a salt thereof, to an elimination reaction of the carboxy protective group to give a compound of the formula: ##STR16## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each as defined above, or a salt thereof, or
- (4) subjecting a compound of formula: ##STR17## wherein R.sup.2, R.sup.3 R.sup.4 and R.sup.5 are each as defined above, and R.sup.1.sub.a is protected amino, or a salt thereof, to an elimination reaction of the amino protective group, to give a compound of the formula: ##STR18## wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined above, or a salt thereof.
- 5. A pharmaceutical composition which comprises, as an active ingredient, a compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9519883 |
Sep 1995 |
GBX |
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Parent Case Info
This application is a continuation of U.S. application Ser. No. 09/043,578, filed Mar. 26, 1998 U.S. Pat. 5,958,914 which is a 371 of PCT/JP96/02797, filed Sep. 27, 1996.
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Name |
Date |
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4452851 |
Takaya |
Jun 1984 |
|
5958914 |
Kawabata |
Sep 1999 |
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55465 |
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EPX |
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FRX |
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DEX |
8-151386 |
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JPX |
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Entry |
Mochida, Chem Abs 110, 114556, May 1986. |
Continuations (2)
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Number |
Date |
Country |
Parent |
043578 |
Mar 1998 |
|
Parent |
PCTJP9602797 |
Sep 1996 |
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